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Methscopolamine: Drug information

Methscopolamine: Drug information
(For additional information see "Methscopolamine: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Anticholinergic Agent
Dosing: Adult
Peptic ulcer

Peptic ulcer (adjunctive): Oral: Initial: 2.5 mg 30 minutes before meals and 2.5 to 5 mg at bedtime; for severe symptoms demanding prompt relief (abdominal pain or cramping), may initiate with 5 mg 30 minutes before meals and 5 mg at bedtime; adjust dose (increase or decrease) to patient response (30 mg/day has been tolerated in some patients).

Dosage adjustment for concomitant therapy: Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.

Dosing: Kidney Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosing: Hepatic Impairment: Adult

There are no dosage adjustments provided in the manufacturer’s labeling; use with caution.

Dosing: Older Adult

Avoid use (Ref).

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.

Cardiovascular: Palpitation, tachycardia

Central nervous system: Headache, insomnia, flushing, nervousness, drowsiness, dizziness, confusion, fever, CNS stimulation may be produced with large doses

Dermatologic: Dry skin, urticaria

Endocrine & metabolic: Lactation suppressed

Gastrointestinal: Constipation, xerostomia, dry throat, dysphagia, nausea, vomiting, loss of taste

Genitourinary: Impotence, urinary hesitancy, urinary retention

Neuromuscular & skeletal: Weakness

Ocular: Blurred vision, cycloplegia, ocular tension increased, pupil dilation

Respiratory: Dry nose

Miscellaneous: Allergic reaction, diaphoresis decreased, hypersensitivity reactions, anaphylaxis

Contraindications

Hypersensitivity to methscopolamine, any component of the formulation, or related drugs; glaucoma; obstructive uropathy (eg, bladder neck obstruction due to prostatic hypertrophy); obstructive disease of the GI tract (eg, pyloroduodenal stenosis); paralytic ileus; intestinal atony of elderly or debilitated patients; unstable cardiovascular status in acute hemorrhage; severe ulcerative colitis; toxic megacolon complicating ulcerative colitis; myasthenia gravis

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: May cause drowsiness and/or blurred vision, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).

• Diarrhea: May be a sign of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy; discontinue treatment if this occurs.

• Heat prostration: May occur in the presence of high environmental temperature; use caution in hot weather and/or exercise.

Disease-related concerns:

• Cardiovascular disease: Use with caution in patients with coronary artery disease, tachyarrhythmias, tachycardia, heart failure or hypertension.

• Hepatic impairment: Use with caution in patients with hepatic impairment.

• Hyperthyroidism: Use with caution in patients with hyperthyroidism.

• Neuropathy: Use with caution in patients with autonomic neuropathy.

• Prostatic hyperplasia: Use with caution in patients with prostatic hyperplasia.

• Renal impairment: Use with caution in patients with renal impairment.

• Ulcerative colitis: Use with caution in patients with ulcerative colitis (large doses may suppress intestinal motility leading to a paralytic ileus); may precipitate/aggravate toxic megacolon.

Special populations:

• Older adult: Use with caution in older adults; increased risk for anticholinergic effects, confusion, and hallucinations.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral, as bromide:

Generic: 2.5 mg, 5 mg

Generic Equivalent Available: US

Yes

Pricing: US

Tablets (Methscopolamine Bromide Oral)

2.5 mg (per each): $2.79 - $2.97

5 mg (per each): $3.97 - $3.98

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Administration: Adult

Oral: Administer 30 minutes before meals and at bedtime.

Use: Labeled Indications

Peptic ulcer (adjunctive): Adjunctive therapy for the treatment of peptic ulcer

Limitations of use: Has not been shown to be effective in contributing to the healing of peptic ulcer, decreasing the rate of recurrence, or preventing complications

Medication Safety Issues
Older Adult: High-Risk Medication:

Beers Criteria: GI antispasmodics with highly anticholinergic activity (methscopolamine) are identified in the Beers Criteria as potentially inappropriate medications to be avoided in patients 65 years and older (independent of diagnosis or condition) due to their highly anticholinergic properties and uncertain effectiveness as an antispasmodic (Beers Criteria [AGS 2023]).

International issues:

Pamine [US, Canada] may be confused with Pemine brand name for penicillamine [Italy]

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Acetylcholinesterase Inhibitors: May diminish the therapeutic effect of Anticholinergic Agents. Anticholinergic Agents may diminish the therapeutic effect of Acetylcholinesterase Inhibitors. Risk C: Monitor therapy

Aclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Amantadine: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Anticholinergic Agents: May enhance the adverse/toxic effect of other Anticholinergic Agents. Risk C: Monitor therapy

Botulinum Toxin-Containing Products: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Cannabinoid-Containing Products: Anticholinergic Agents may enhance the tachycardic effect of Cannabinoid-Containing Products. Risk C: Monitor therapy

Chloral Betaine: May enhance the adverse/toxic effect of Anticholinergic Agents. Risk C: Monitor therapy

Chlorprothixene: Anticholinergic Agents may enhance the anticholinergic effect of Chlorprothixene. Risk C: Monitor therapy

Cimetropium: Anticholinergic Agents may enhance the anticholinergic effect of Cimetropium. Risk X: Avoid combination

CloZAPine: Anticholinergic Agents may enhance the constipating effect of CloZAPine. Management: Consider alternatives to this combination whenever possible. If combined, monitor closely for signs and symptoms of gastrointestinal hypomotility and consider prophylactic laxative treatment. Risk D: Consider therapy modification

Eluxadoline: Anticholinergic Agents may enhance the constipating effect of Eluxadoline. Risk X: Avoid combination

Gastrointestinal Agents (Prokinetic): Anticholinergic Agents may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic). Risk C: Monitor therapy

Glucagon: Anticholinergic Agents may enhance the adverse/toxic effect of Glucagon. Specifically, the risk of gastrointestinal adverse effects may be increased. Risk C: Monitor therapy

Glycopyrrolate (Oral Inhalation): Anticholinergic Agents may enhance the anticholinergic effect of Glycopyrrolate (Oral Inhalation). Risk X: Avoid combination

Glycopyrronium (Topical): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Ipratropium (Oral Inhalation): May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Itopride: Anticholinergic Agents may diminish the therapeutic effect of Itopride. Risk C: Monitor therapy

Levosulpiride: Anticholinergic Agents may diminish the therapeutic effect of Levosulpiride. Risk X: Avoid combination

Mianserin: May enhance the anticholinergic effect of Anticholinergic Agents. Risk C: Monitor therapy

Mirabegron: Anticholinergic Agents may enhance the adverse/toxic effect of Mirabegron. Risk C: Monitor therapy

Nitroglycerin: Anticholinergic Agents may decrease the absorption of Nitroglycerin. Specifically, anticholinergic agents may decrease the dissolution of sublingual nitroglycerin tablets, possibly impairing or slowing nitroglycerin absorption. Risk C: Monitor therapy

Opioid Agonists: Anticholinergic Agents may enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination. Risk C: Monitor therapy

Oxatomide: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Potassium Chloride: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Chloride. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium chloride. Risk X: Avoid combination

Potassium Citrate: Anticholinergic Agents may enhance the ulcerogenic effect of Potassium Citrate. Management: Patients on drugs with substantial anticholinergic effects should avoid using any solid oral dosage form of potassium citrate. Risk X: Avoid combination

Pramlintide: May enhance the anticholinergic effect of Anticholinergic Agents. These effects are specific to the GI tract. Risk X: Avoid combination

Ramosetron: Anticholinergic Agents may enhance the constipating effect of Ramosetron. Risk C: Monitor therapy

Revefenacin: Anticholinergic Agents may enhance the anticholinergic effect of Revefenacin. Risk X: Avoid combination

Rivastigmine: Anticholinergic Agents may diminish the therapeutic effect of Rivastigmine. Rivastigmine may diminish the therapeutic effect of Anticholinergic Agents. Management: Use of rivastigmine with an anticholinergic agent is not recommended unless clinically necessary. If the combination is necessary, monitor for reduced anticholinergic effects. Risk D: Consider therapy modification

Secretin: Anticholinergic Agents may diminish the therapeutic effect of Secretin. Management: Avoid concomitant use of anticholinergic agents and secretin. Discontinue anticholinergic agents at least 5 half-lives prior to administration of secretin. Risk D: Consider therapy modification

Thiazide and Thiazide-Like Diuretics: Anticholinergic Agents may increase the serum concentration of Thiazide and Thiazide-Like Diuretics. Risk C: Monitor therapy

Tiotropium: Anticholinergic Agents may enhance the anticholinergic effect of Tiotropium. Risk X: Avoid combination

Topiramate: Anticholinergic Agents may enhance the adverse/toxic effect of Topiramate. Risk C: Monitor therapy

Umeclidinium: May enhance the anticholinergic effect of Anticholinergic Agents. Risk X: Avoid combination

Pregnancy Considerations

Animal reproduction studies have not been conducted. Methscopolamine is a derivative of scopolamine. Scopolamine is reported to cross the placenta; fetal toxicity noted in case reports.

Breastfeeding Considerations

It is not known if methscopolamine is excreted in breast milk. Anticholinergics may suppress lactation. The manufacturer recommends that caution be exercised when administering methscopolamine to nursing women.

Dietary Considerations

Take 30 minutes before meals and at bedtime.

Monitoring Parameters

Follow by upper GI contrast radiology or endoscopy to ensure healing

Mechanism of Action

Methscopolamine is a quaternary ammonium derivative of scopolamine that exerts anticholinergic effects, which include reducing the volume and total acid content of gastric secretion, inhibiting gastrointestinal motility and salivary secretion, dilation of the pupil, and inhibition of accommodation that results in blurring of vision.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: ~1 hour

Duration: 4 to 6 hours

Absorption: Poorly and unreliably absorbed

Bioavailability: 10% to 25%

Excretion: Bile and urine; feces (as unabsorbed drug)

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (CN) China: Methscopolamine bromide | Scopolamine;
  • (DE) Germany: Holopon;
  • (GB) United Kingdom: Pamine;
  • (HK) Hong Kong: Buscopon | Holpin | L-Scopolamine-N-Methylbromide | Neo copan | Scopolamine | Scopolamine methylbromide | U metamine;
  • (ID) Indonesia: Holopon;
  • (MY) Malaysia: Encodex;
  • (PR) Puerto Rico: Methscopolamine bromide | Pamine | Pamine forte;
  • (SA) Saudi Arabia: Holopon;
  • (SG) Singapore: Holopon;
  • (TW) Taiwan: Buscon
  1. 2023 American Geriatrics Society Beers Criteria Update Expert Panel. American Geriatrics Society 2023 updated AGS Beers Criteria for potentially inappropriate medication use in older adults. J Am Geriatr Soc. 2023;71(7):2052-2081. doi:10.1111/jgs.18372 [PubMed 37139824]
  2. Methscopolamine bromide (tablets) [prescribing information]. Irvine, CA: Nexgen Pharma; January 2020.
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